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Assay Detail

CHEMBL3382832

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Inhibition of LPS-induced IL6 production in human PBMC after 18 to 24 hrs by immunoassay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type PBMC
Confidence 1 — Organism
Curated By Autocuration

Target

PBMC (CHEMBL613107)
Type CELL-LINE
Organism Homo sapiens

Publication

The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor.
Gosmini R, Nguyen VL, Toum J, Simon C, Brusq JM, Krysa G, Mirguet O, Riou-Eymard AM, Boursier EV, Trottet L, Bamborough P, Clark H, Chung CW, Cutler L, Demont EH, Kaur R, Lewis AJ, Schilling MB, Soden PE, Taylor S, Walker AL, Walker MD, Prinjha RK, Nicodème E.
J Med Chem (2014) 57 : 8111 -8131
PubMed 25249180 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.90 8.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3353992 1 8.50
CHEMBL2177300 1 7.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3353992 IC50 = 3.162 nM 8.50
CHEMBL2177300 IC50 = 50.12 nM 7.30